Week 4 (Exam 1) Flashcards

1
Q

Statin Lipid Lowering MOA

A

blocks HMG CoA Reductase to mevalonic acid

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2
Q

Statin Inflammation reducing MOA

A

Reduces CRP and Erythrocyte Sedimentation Rate

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3
Q

Statin Reversal of Endothelial Dysfunction MOA

A
Increase in NO synthesis
Reduced oxidized LDL
Inhibition of Endothelin synthesis
Reduction in Endothelial Permeability to LDL cholesterol
Inactivation of Superoxide
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4
Q

Statin Decreased Thrombogenicity MOA

A

Reduced endothelial and atherosclerotic plaque macrophage tissue factor expression
Decreased Prothrombin activation and thrombin generation
Improved fibrinolysis
Decreased platelet activation

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5
Q

Advicor

A

Lovastatin and Niastatin

XR

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6
Q

Simcor

A

Simvistatin and Niastatin

XR

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7
Q

Vytorin

A

Simbistatin and Ezetimibe

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8
Q

Muscle related side effects of Statin

A

Bilateral, symmetrical, skeletal muscle myopathy

No rise in Creatine Kinase

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9
Q

How do statins cause liver damage?

A

Temporary depletion of intracellular cholesterol causes an increase in LDL receptor production

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10
Q

Statins and transaminase levels

A

Asx and dose-related increases 3x normal

ALT > AST (distinguishes liver from muscle AST)

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11
Q

All statins have been show to cause…

A

AKI (rhabdomyolysis, subsequent myoglobinemia)

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12
Q

The two pro-drug Statins

A

Simvistatin and Lovastatin (increases their hepatic metabolism)

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13
Q

Statins that should maybe be given at a lower dose for asian populations

A

Rosuvastatin and Simvastatin

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14
Q

Statins metabolized in CYP3A4 pathway

A

Atorvastain
Simvastatin
Lovastatin

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15
Q

Statins metabolized in CYP2C9

A

Fluvastatin

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16
Q

Ezetimibe MOA

A

Inhibits dietary and biliary cholesterol absorption at brush border via NPC1L1 so Liver has to then take more from the circulation
Also blocks chostesterol traffickers Aminopeptidase N and Cave-in 1-Annexin A2 Complex

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17
Q

NPC1A1

A

Expressed in Intestine and Liver as Sterol Transporter to mediate intestinal cholesterol absorption and counterbalances hepatobiliary cholesterol excretion
Inhibited by Ezetimibe

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18
Q

Indications for Ezetimibe

A

Homozygous Familial Hypocholeterolemia
Homozygous Sitosterolemia
Primary Hyperlipidemia

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19
Q

Ezetimibe dosing for Homozygous Familial Hypercholesterolemia

A

10mg PO qDay w/ Atorvastatin or Simvastatin

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20
Q

Ezetimibe dosing in Primary Hyperlipidemia

A

10mg PO qDay w/ HMG-CoA Reductase inhibitors in diet
Can be monotherapy
can be w/ fenofibrate
can be w/ Statins

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21
Q

Contraindications of Ezetimibe

A

Pregnancy and breastfeeding when combo w/ statin

Hepatic Disease or impairment

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22
Q

Toxicity of Ezetimibe

A

Skeletal muscle toxicity when used with statin, especially over 65 y.o., hypothyroidism, renal impairment

23
Q

PCSK9 Inhibitor MOA

A

Serine Protease: cleaves LDL receptors at Serine Residues (degrades them)
Increases Hepatic LDL-R and Decreases Plasma LDL-C

24
Q

The two PCSK9 Inhibitors

A

Alirocumab and Evolocumab

25
Q

Indications for Alirocumab and Evolocumab

A

PCSK9 Inhibitors: Tx FH and Atherosclerotic CVD

26
Q

Most common PCSK9-I side effects

A

Runny nose, sore throat, injection site rxn

27
Q

Bile Acid Sequestrant MOA

A

Not absorbed, but bind bile acids and are excreted as a complex
Cholesterol depletion increases LDL rec Activity (increases removal of LDL cholesterol from blood)

28
Q

Bile Acid Sequestrants (3)

A

Colesevelam, Colestipol, Cholestyramine

29
Q

Contraindications of Bile Acid Sequestrants

A

Its with Dysbetalipoproteinemia: induced Pancreatitis

Decreased GI Motility

30
Q

Adverse Effects of Bile Acid Sequestrations

A

Elevated TAGs
Elevated Liver Enzymes
Vit D Deficiency

31
Q

Bile Acid Sequestrant Warnings and Precautions

A

ADEK and Folic Acid Deficiency

Phenylketonuria (contains F)

32
Q

Fibrate MOA

A

PPARa Activator: Increases liver enzymes for TAG metabolism and uptake

33
Q

Fenofibric Acid (Fibrate) Indications

A

Dyslipidemia

Severe HyperTAG-emia

34
Q

Gemfibrozil (fibrate) Indications

A

Severe HyperTAG-emia

Primary Prevention of Coronary Heart Disease (in type IIb patients)

35
Q

Gemfibrozil Drug Contraindications

A
Dasabuvir
Repaglinide
Simvastatin (muscle toxicity with statins)
Cerivastatin
Enzalutamide (increases seizure risk)
Selexipag
36
Q

Gemfibrozil Side Effects

A

GI: stomach pain, nausea
Increased liver enzymes (same with other Fibrates)
Elevated Creatinine Kinase (like other Fibrates)
Gallstones (like other Fibrates), maybe.
Myopathy and Rhabdomyolysis (like other Fibrates)
Kidney and Liver Dz

37
Q

Fibrates and GFR

A

Do not use if GFR is below 30 ml/min

GFR between 30 - 59? Keep dose below 54 mg/day

38
Q

Why can Fibrates cause a slight increase in serum creatinine?

A

They inhibit kidney Organic Cation Transporter 2

39
Q

Gemfibrozil is a strong inhibitor of:

A

CYP2C8

40
Q

Bile Acid Sequestrants and Fibrates

A

Can interfere with Fibrates (take 1 hour before or 4 hours after BAS)

41
Q

Colchicine + Fibrates

A

Muscle Toxicity, Rhabdomyolysis

42
Q

Fibrates + Ezetimibe

A

Fibrates increase the levels of Ezetimibe

43
Q

Fibrates + Warfarin

A

Fibrates interfere with the warfarin

44
Q

Fibrates + Cyclosporine / Tacrolimus

A

Nephrotoxicity

45
Q

OAT1B1

A

Inhibited by Gemfibrozil (hepatic uptake transporter)

46
Q

Fibrates in pregnancy

A

Idk, but definitely don’t use them while nursing

47
Q

Niacin MOA

A

Maybe increase lipoprotein lipase
Maybe inhibits release of free fatty acids from adipose
Maybe decreases rate of LDL/VLDL synthesis

48
Q

Indications for Niacor

A

Reduction of total and LDL Cholesterol

Adjunct therapy for adults wit super high TAGs

49
Q

Indications for Niaspan

A

To increase HDL

To reduce total cholesterol, LDL, Apo B, TAGs

50
Q

Niacin Adverse Effects

A

Flushing, itching
Blood sugar elevation
Raise Uric Acid Levels, liver enzymes

51
Q

Niacin warnings and precautions

A
Don't use with Liber Disease
Can raise blood sugar: don't use with diabetes
Can increase uric acid levels (gout)
Can prolong bleeding time
Contraindicated in PUD
52
Q

Niacin metabolism

A

CYP2D6 Inhibitor

53
Q

Drug interactions with Niacin

A

Statins and Bile Acid Sequestrants